PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND

FLUOROQUINOLONES

LEARNING OBJECTIVES  Excretion: Mainly excreted through the bile; Renal

 Describe the pharmacokinetics and pharmacodynamics excretion is only 5%
of erythromycin.
 Apply the nursing process for tetracyclines, including Pharmacodynamics
patient teaching.  Clarithromycin: Twice a day dosing; acid stable with
 Summarize the nurse’s role in detecting ototoxicity and better GI absorption than erythromycin.
nephrotoxicity associated with the administration of  Azithromycin: Once a day dosing; needs to be given 2
aminoglycosides. hrs before or after a meal.
 Explain the importance for ordering peak and trough  Erythromycin: oral preparation 1 hr; peak concentration
concentration levels for aminoglycosides. is 4 hr; action is 6 hrs.
 Develop a teaching plan for a patient prescribed a
fluoroquinolone (quinolone). Side effects and Adverse Effects
 Contrast the nursing interventions for each of the drug  GI disturbances (nausea, vomiting, diarrhea, and
categories: macrolides, tetracyclines, aminoglycosides, and abdominal cramps)
fluoroquinolones.  Conjunctivitis (azithromycin)
 Allergic reactions (erythromycin)
KEY TERMS  Hepatoxicity (liver toxicity) - erythromycin and
BACTERICIDAL  To kill bacteria. azithromycin are taken in high doses with other hepatotoxic
BACTERIOSTATIC  Inhibit bacterial growth. drugs.
HEPATOTOXICITY  Liver toxicity.  Liver damage
NEPHROTOXICITY  Kidney toxicity.
 Develops hearing or balance Drug Interaction
OTOTOXICITY  Macrolides can increase serum levels of theophylline
problems.
 Microorganism capable of (bronchodilator), carbamazepine (anticonvulsant), and
PATHOGEN warfarin (anticoagulant).
producing disease.
PHOTOSENSITIVITY  Sunburn reaction.  Erythromycin should not be used with other macrolides.
 Secondary infection resulting drug  Antacids may reduce azithromycin peak.
SUPERINFECTION
theraphy.
Refer to Table.1, Table.2, and Table.3
MACROLIDES, LINCOSAMIDES, GLYCOPEPTIDES,
LINCOSAMIDES
AND KETOLIDES
Examples of lincosamides:
 Clindamycin (Cleocin), is widely prescribed since
MACROLIDES 
it is absorbed better.
Broad-spectrum antibiotics
 Lincomycin (Lincocin)
 azithromycin (Zithromax)
Lincosamides are derivatives of an amino acid and a
 clarithromycin (Biaxin) 
sulfur-containing octose.
  erythromycin (E-Mycin), the first macrolide, was
Lincosamides, macrolides, and chloramphenicol,
derived from the fungus-like bacteria
 although not structurally related, seem to act at this
Streptomyces erythreus and was first introduced
same site.
in the early 1950s.
The lincosamides are bacteriostatic or bactericidal
 Route: IV and Oral 
depending on the concentration.
Low to moderate drug doses(bacteriostatic effect);

high drug doses (bactericidal effect). Side effects and Adverse Effects
Gastric acid destroys erythromycin in the stomach;  GI irritation (nausea, vomiting, and stomatitis)
 therefore, acid-resistant salts are added to  The rash may occur.
erythromycin to decrease dissolution in the stomach.  Colitis
Active (gram-positive bacteria); Moderately active  Anaphylactic shock.

(gram-negative bacteria).
Treats mild to moderate infections of the respiratory Drug Interaction
tract, sinuses, gastrointestinal (GI) tract, skin and soft  Clindamycin and lincomycin are incompatible with

tissue, diphtheria, impetigo contagiosa, and sexually aminophylline, phenytoin (Dilantin), barbiturates, and
transmitted infections (STIs). ampicillin.

Pharmacokinetics Refer to Table.1

 Absorption: Destroyed by the gastric juice so better
given as an enteric coated tablet or in stearate form.

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

GLYCOPEPTIDES
Examples of glycopeptides are: KETOLIDES
 Vancomycin(Vancocin)  Sstructurally related to macrolides.
 used in the 1950s to treat staphylococcal Telithromycin (Ketek)
infections  18 years and above

 used against S. aureus  treat mild to moderate community-acquired

 cardiac surgical prophylaxis pneumonia.
 Telavancin(Vibativ)
 treats selected gram-positive bacteria.
Pharmacokinetics
 skin infections
 Telithromycin (orally; absorbed by the GI tract)
 once-daily dosing
 It is excreted in the feces and urine.
 It is 60% to 70% protein-bound, and the half-life is 10
Pharmacokinetics hours.
 Vancomycin when given orally:
 not absorbed systematically Pharmacodynamics
 excreted in feces  Telithromycin inhibits protein synthesis in
 staphylococcal enterocolitis microorganisms by binding to the bacterial ribosomal RNA
 clostridium difficile site of the 50S subunit, resulting in bacterial cell death. The
 Vancomycin when given IV: peak action is 1 hour.
 MRSA; septicemia; bone, skin, and lower
respiratory tract infections. Side effects and Adverse Effects
 excreted in urine.  Visual disturbances (blurred vision and diplopia)
 Headache and dizziness
Pharmacodynamics  Altered taste, nausea, vomiting, diarrhea
 Vancomycin inhibits bacterial cell wall synthesis and is  Liver failure
active against several gram-positive microorganisms. The  Myasthenia gravis
peak action is 30 minutes after the end of the infusion.
Drug Interaction
Side effects and Adverse Effects  Telithromycin levels are increased when taken
 Vancomycin (nephrotoxicity and ototoxicity) concurrently with antilipidemics (simvastatin, lovastatin, and
 chills, dizziness, fever, rashes, nausea, vomiting, and atorvastatin), itraconazole, ketoconazole, and
thrombophlebitis(injection site). benzodiazepines.
 Rapid IV ("red man" syndrome or red neck syndrome)  Blood levels of telithromycin are decreased when taken
 red blotching of the face, neck, and chest. with rifampin, phenytoin, carbamazepine, or phenobarbital,
 Eosinophia, neutropenia, and Stevens Johnson syndrome. producing a subtherapeutic level.
 Severe hypotension, tachycardia, tingling, and cardiac
arrest.
Refer to Table.1
Drug Interaction
 Dimenhydrinate (Dramamine) can mask ototoxicity when
TETRACYCLINES
taken with vancomycin.
 The risk of nephrotoxicity and cytotoxicity (furosemide,
aminoglycosides, amphotericin B, colistin, cisplatin, and TETRACYCLINES
cyclosporine).  Isolated from streptomyces aureofaciens in 1948.
Decreased absorption of oral vancomycin (cholestyramine First broad-spectrum antibiotics (gram-positive and
and colestipol).  gram-negative).

Refer to Table.1 Act by inhibiting bacterial protein synthesis and have


a bacteriostatic effect.
Combined with (metronidazole, and bismuth

subsalicylate) treat helicobacter pylori.
 At low doses (minimizes toxic effect).
Continuous use results in bacterial resistance to

drugs.

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES
Should not be taken with magnesium and aluminum
antacid preparations, calcium, or iron-containing
 tigecycline.
drugs.
Absorption of doxycycline and minocycline (food

ingestion).
Side effects and Adverse Effects
 GI disturbances (nausea, vomiting, and diarrhea).
 Photosensitivity (sunburn reaction);
Demeclocycline(Declomycin).
 1st-trimester pregnancy; teratogenic effects.
 Discoloration of teeth (last term pregnancy and 8 yrs
old).
 Minocycline (Minocin)- difficulty in balance.
 High dose with nephrotoxic drugs; Nephrotoxicity.
 Superinfection.
Drug Interaction
 Antacids (Maalox) and iron-containing drugs.
 Milk and high drugs in calcium.
 Should be taken two hrs after tetracycline.
 Doxycycline and minocycline absorbers in the GI tract
are better with milk products and food.
 Administering tetracycline with an aminoglycoside may
increase the risk of nephrotoxicity.
Refer to Table.4, Table.5, and Table.6
GLYCYLCYCLINES
GLYCYLCYCLINES
Tigecycline (Tygacil) is an antibiotic in the category

of glycylcycline.
Acts by blocking protein synthesis in bacterial cells

(bacteriostatic action).
Indications: complicated skin infections and
intraabdominal infections (Staphylococcus aureus,

Escherichia coli, Streptococcus pyogenes, Klebsiella
pneumoniae, and Clostridium perfringens).
Side effects and Adverse Effects
 GI tract (nausea, vomiting, abdominal pain, and diarrhea).
 Pseudomembranous colitis (rare).
 Photosensitivity
 Headache, dizziness, and insomnia.
 Hypertension, hypotension, anemia, leukocytosis, and
thrombocythemia.
 Hyperglycemia, hypokalemia, and elevated BUN.
 Elevated liver enzymes.
Drug Interaction
 Oral contraceptives may be less effective when given
concurrently with tigecycline. Warfarin levels may be
increased and may lead to bleeding when taken with
Refer to Table.6
AMINOGLYCOSIDES
AMINOGLYCOSIDES
Aminoglycosides act by inhibiting bacterial protein

synthesis.
Used against gram-negative bacteria such as E. coli,

Proteus spp., and Pseudomonas spp.
Streptomycin sulfate, derived from the bacterium
Streptomyces griseus in 1944,
  used to treat tuberculosis.
 tularemia and bubonic pneumonic forms of
plague.
 Aminoglycosides are for serious infections.
Cannot be absorbed from the GI tract and cannot

cross into the cerebrospinal fluid.
These agents are primarily administered IM and IV,

(e.g., neomycin, paromomycin)
Neomycin is frequently used as a preoperative bowel

antiseptic.
Paromomycin is useful in treating intestinal amebiasis

and tapeworm infestation.
Currently used to treat Pseudomonas aeruginosa
infection including gentamicin, tobramycin, and

amikacin. P. aeruginosa is sensitive to gentamicin.
Amikacin (gentamicin and tobramycin).
Pharmacokinetics
 Gentamicin is administered IM and IV. This drug has a
short half-life, and the drug dose can be given three to
four times a day. Excretion of this drug is primarily
unchanged in the urine.
Pharmacodynamics
 Gentamicin inhibits bacterial protein synthesis and has a
bactericidal effect.
 Gentamicin has a pregnancy category of C.
 Onset of action is rapid or immediate.
 Peak action for gentamicin is 1 to 2 hours.
 Usually administered as IV.
 Patient’s blood levels are drawn periodically to
determine the drug’s peak blood level and trough level.
Side effects and Adverse Effects
 Ototoxicity
 Nephrotoxicity
 Superinfection
.
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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Drug Interaction
 Penicillins, desired effects are greatly decreased.
 Warfarin (Coumadin) can increase the desired effect.
 The risk of ototoxicity increases when ethacrynic acid
and aminoglycoside are given.
Refer to Table.7, Table 8, and Table.9
FLUOROQUINOLONES
FLUOROQUINOLONES
The mechanism of action of fluoroquinolones is to
interfere with the enzyme DNA gyrase, which is
needed to synthesize bacterial deoxyribonucleic acid

(DNA). Their antibacterial spectrum includes
bactericidal action on both gram-positive and gram-
negative organisms.
Nalidixic acid (NegGram) and cinoxacin (Cinobac) are
the earliest derivatives of the fluoroquinolone group,
(for urinary tract infection).

 no longer available on the market in the United
States.
Effective against some gram-positive organisms,
such as Streptococcus pneumoniae, and against
  The pregnancy category is B.
Haemophilus influenzae, P. aeruginosa, Salmonella,
and Shigella.
Useful in the treatment of urinary tract, bone, and
joint infections; bronchitis; pneumonia;
gastroenteritis; and gonorrhea.
 Ciprofloxacin (Cipro) and norfloxacin (Noroxin)
 are synthetic antibacterials related to nalidixic
acid.
 Moxifloxacin (Avelox) is available for once-a-
day oral and parenteral dosing.
Pharmacokinetics
 Levofloxacin (Levaquin) is well absorbed from the GI
tract. It has a low protein-binding effect of 50% and a
moderately short half-life of 6 to 8 hours. Levofloxacin is
excreted unchanged in the urine.
Pharmacodynamics
 Inhibits bacterial DNA synthesis
 A high tissue distribution; should be taken before meals
 Antacids also decrease the absorption rate.
 Levofloxacin (oral hypoglycemics, theophylline, and
caffeine).
 The onset of action of 0.5 to 1 hour; peak concentration
time is 1 to 2 hours.
LIPOPEPTIDES
LIPOPEPTIDES
Daptomycin (Cubicin) is an FDA-approved.
 Acts by binding to the bacterial membrane;
causing rapid depolarization of its membrane
potential, inhibiting protein, DNA, and RNA
 synthesis.
 Indications; complicated skin infections due to
gram-positive microorganisms, septicemia due
to Staphylococcus aureus infections, and
infective endocarditis due to MRSA.
Pharmacokinetics
 Administered through IV
 After gentle rotation of vial to ensure dilution, further,
dilute in 50 to 100 mL of NS and administer over 30
minutes. However, it should not be mixed with dextrose-
containing diluents.
 The protein-binding capacity is 92%,with a half-life of 8
hours.
 Primarily excreted by the kidneys.
Pharmacodynamics
 Daptomycin binds to the bacterial membrane and causes
cell death. An effective trough concentration of 5.9
mcg/mL is usually achieved by the third dose.
Side effects and Adverse Effects
 Hypertension, hypotension, anemia, numbness, tingling,
dizziness, insomnia.
 Pain or burning on urination
 Nausea, vomiting, diarrhea, constipation, and pallor.
 Chest pain, hypokalemia, hyperkalemia, hyperglycemia,
hypoglycemia, bleeding, rhabdomyolysis, and pleural
effusion.
Drug Interaction
 Given with HMG-CoA reductase inhibitors, the risk of
rhabdomyolysis is increased.
 Daptomycin toxicity may be increased when given
concurrently with tobramycin.
 Warfarin may lead to increased bleeding when taken
with daptomycin.

Refer to Table.10, Table.11, and Table.12

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

UNCLASSIFIED ANTIBACTERIAL DRUGS

 Chloramphenicol
 Spectinomycin
 Quinupristin/dalfopristin (Synercid)

Chloramphenicol
 Discovered in 1947.
Bacteriostatic action by inhibiting bacterial protein

synthesis.
 It is used only to treat serious infections.
Effective against gram-negative and gram-positive

bacteria and many other microorganisms.

Spectinomycin
An aminocyclitol antibiotic used to treat susceptible

strains of Neisseria gonorrhoeae.
 Produced by Streptomyces spectabilis.
Active against gram-negative bacteria and used for

the treatment of gonorrhea.

Quinupristin/Dalfopristin (Synercid)
Effective for treating (VREF) bacteremia and skin

infected by S. aureus and S. pyogenes.
Acts by disrupting the protein synthesis of the

organism.
When administering the drug through a peripheral IV

line (pain, edema, and phlebitis).

Refer to Table.10

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.1

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.2

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.3

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.4

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.5

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.6

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.7

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.8

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.9

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.10

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.11

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PHARMACOLOGY: MACROLIDES, TETRACYCLINES, AMINOGLYCOSIDE AND
FLUOROQUINOLONES

Table.12

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